Substituted pyrazoles
First Claim
Patent Images
1. Use of the compounds of the formula I in which X denotes CH or N, R1 denotes H, A, Hal, (CF2)nHet, (CH2)nAr, cycloalkyl having 3 to 7 C atoms, CF3, NO2, CN, C(NH)NOH or OCF3, R2 denotes (CH2)nHet, (CH2)nAr, cycloalkyl having 3 to 7 C atoms or CF3, R3, R4 denote H, (CH2)nCO2R5, (CH2)nCOHet, (CH2)nCON(R5)2, (CH2)n000(CH2)nHet, CHO, (CH2)nOR5, (CH2)nHet, (CH2)nN(R5)2, CH═
- N—
OA, CH2CH═
N—
OA, (CH2)nNHOA, (CH2)nN(R5)Het, (CH2)nCH═
N-Het, (CH2)n000R5, (CH2)nN(R5)CH2CH2OR5, (CH2)nN(R5)CH2CH2OCF3, (CH2)nN(R5)C(R5)H000R5, (CH2)nN(R5)CH2COHet, (CH2)nN(R5)CH2Het, (CH2)nN(R5)CH2CH2Het, (CH2)nN(R5)CH2CH2N(R5)CH2000R5, (CH2)nN(R5)CH2CH2OR5, (CH2)nN(R5)CH2CH2N(R5)2, CH═
CH000R5, CH═
CHCH2NR5Het, CH═
CHCH2N(R5)2, CH═
CHCH20R5, CH═
CHCH2Het, (CH2)nN(R5)Ar, (CH2)nN(000R)COOR5, (CH2)nN(CONH2)000R5, (CH2)nN(CONH2)CONH2, (CH2)nN(CH2000R)COOR5, (CH2)nN(CH2CONH2)000R5, (CH2)nN(CH2CONH2)CONH2, (CH2)nCHR5COR5, (CH2)nCHR5000R5, (CH2)nCHR5CH20R5, where in each case one of the radicals R3 or R4 has the meaning H, R5 denotes H or A A denotes straight-chain or branched alkyl or cycloalkyl having 2 to 4 C atoms, having 1 to 10 C atoms, alkenyl having 2 to 10 C atoms, alkoxyalkyl having 2 to 10 C atoms or cycloalkyl having 4 to 7 C atoms, each of which is unsubstituted or substituted by Hal or CN, Het preferably denotes a saturated, unsaturated or aromatic mono or bicyclic heterocyclic radical having 1 to 15 C atoms which is unsubstituted or mono- or polysubstituted by A and/or Hal or a linear radical having 1 to 15 C atoms containing one or two hetero atoms, Ar denotes a phenyl radical which is unsubstituted or mono or polysubstituted by A and/or Hal, ORt, OOCR5, COORS, CON(R5)2, CN, NO2, NH2, NHCOR5, CF3 or SO2CH3, n denotes 0, 1, 2, 3, 4 or 5 and Hal denotes F, Cl, Br or I, and salts and solvates, enantiomers and racemates thereof for the preparation of a medicament for the treatment and prophylaxis of diseases which can be influenced by the binding of the compounds of the formula I to 5 HT receptors.
1 Assignment
0 Petitions
Accused Products
Abstract
The compounds of the formula (I) and salts and solvates thereof, in which X, R1, R2, R3, R4 and R5 have the meanings indicated in Claim (1), are suitable as ligands of 5 HT receptors.
-
Citations
10 Claims
-
1. Use of the compounds of the formula I
in which X denotes CH or N, R1 denotes H, A, Hal, (CF2)nHet, (CH2)nAr, cycloalkyl having 3 to 7 C atoms, CF3, NO2, CN, C(NH)NOH or OCF3, R2 denotes (CH2)nHet, (CH2)nAr, cycloalkyl having 3 to 7 C atoms or CF3, R3, R4 denote H, (CH2)nCO2R5, (CH2)nCOHet, (CH2)nCON(R5)2, (CH2)n000(CH2)nHet, CHO, (CH2)nOR5, (CH2)nHet, (CH2)nN(R5)2, CH═ - N—
OA, CH2CH═
N—
OA, (CH2)nNHOA, (CH2)nN(R5)Het, (CH2)nCH═
N-Het, (CH2)n000R5, (CH2)nN(R5)CH2CH2OR5, (CH2)nN(R5)CH2CH2OCF3, (CH2)nN(R5)C(R5)H000R5, (CH2)nN(R5)CH2COHet, (CH2)nN(R5)CH2Het, (CH2)nN(R5)CH2CH2Het, (CH2)nN(R5)CH2CH2N(R5)CH2000R5, (CH2)nN(R5)CH2CH2OR5, (CH2)nN(R5)CH2CH2N(R5)2, CH═
CH000R5, CH═
CHCH2NR5Het, CH═
CHCH2N(R5)2, CH═
CHCH20R5, CH═
CHCH2Het, (CH2)nN(R5)Ar, (CH2)nN(000R)COOR5, (CH2)nN(CONH2)000R5, (CH2)nN(CONH2)CONH2, (CH2)nN(CH2000R)COOR5, (CH2)nN(CH2CONH2)000R5, (CH2)nN(CH2CONH2)CONH2, (CH2)nCHR5COR5, (CH2)nCHR5000R5,(CH2)nCHR5CH20R5, where in each case one of the radicals R3 or R4 has the meaning H, R5 denotes H or A A denotes straight-chain or branched alkyl or cycloalkyl having 2 to 4 C atoms, having 1 to 10 C atoms, alkenyl having 2 to 10 C atoms, alkoxyalkyl having 2 to 10 C atoms or cycloalkyl having 4 to 7 C atoms, each of which is unsubstituted or substituted by Hal or CN, Het preferably denotes a saturated, unsaturated or aromatic mono or bicyclic heterocyclic radical having 1 to 15 C atoms which is unsubstituted or mono- or polysubstituted by A and/or Hal or a linear radical having 1 to 15 C atoms containing one or two hetero atoms, Ar denotes a phenyl radical which is unsubstituted or mono or polysubstituted by A and/or Hal, ORt, OOCR5, COORS, CON(R5)2, CN, NO2, NH2, NHCOR5, CF3 or SO2CH3, n denotes 0, 1, 2, 3, 4 or 5 and Hal denotes F, Cl, Br or I, and salts and solvates, enantiomers and racemates thereof for the preparation of a medicament for the treatment and prophylaxis of diseases which can be influenced by the binding of the compounds of the formula I to 5 HT receptors. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10)
- N—
Specification